CX08005 is a competitive PTP1B inhibitor (IC50 = 0.781 μM). Binds catalytic P-loop of enzyme. Improves insulin sensitivity in obese mice in the glucose tolerance test and the homeostasis model assessment of insulin resistance index (HOMVIP(LA)IR). Enhances insulin-induced glucose uptake in adipocytes and myotubes in vitro. Exhibits some selectivity for PTP1B over other protein tyrosine phosphatases, except TCPTP.
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